US6319938B1ExpiredUtility

Prophylactic or therapeutic drug for renal diseases

49
Assignee: TAKEDA CHEMICAL INDUSTRIES LTDPriority: Apr 22, 1993Filed: Dec 20, 1999Granted: Nov 20, 2001
Est. expiryApr 22, 2013(expired)· nominal 20-yr term from priority
A61P 3/08A61P 3/10A61P 29/00A61K 31/415A61P 15/00A61P 13/02A61K 31/4184A61P 13/12A61K 31/4245Y02A50/30
49
PatentIndex Score
4
Cited by
31
References
17
Claims

Abstract

Prophylactic or therapeutic drugs for diabetic nephropathy or glomerulonephritis, comprising, as an active ingredient, a compound or salt thereof represented by formula (I)wherein R1 stands for H or an optionally substituted hydrocarbon residue; R2 stands for an optionally esterified carboxyl group; R3 stands for a group actually or potentially capable of forming an anion; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic chain length of two or less; n stands for 1 or 2; ring A stands for a benzene ring having an optional substituent in addition to R2; Y stands for a bond, -O-, -S(O)m-, wherein m stands for 0, 1 or 2, or -N(R4)- wherein R4 stands for H or an optionally substituted alkyl group are disclosed.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
       1. A method for tbe prophylaxis or treatment of diabetic nephropathy or glomerulonephritis in a mammal comprising the step of administering a pharmaceutically effective amount of a compound or salt thereof represented by formula (I′)                    
       wherein R 1  stands for H or a lower (C 1 -C 4 ) alkyl, R 2  stands for a group represented by the formula —CO—D″ where D″ stands for hydroxy or a lower (C 1 -C 4 ) alkoxy group, the alkyl moiety of which optionally is substituted with hydroxy, amino, halogen, lower (C 2 -C 6 ) alkanoyloxy, lower (C 4 -C 7 ) cycloalkanoyloxy, lower (C 1 -C 6 ) alkoxyearbonyloxy, lower (C 3 -C 7 ) cycloalkoxycarbonyloxy or lower (C 1 -C 4 ) alkoxy, R 3  stands for a tetrazolyl, carboxyl group or a group represented by the formula:                    
       where i stands for —O— or —S— and j stands for >C═O, >C═S or >S(O) m  where m is 0, 1 or 2; ring A stands for a benzene ring; Y stands for O, N(H) or S, to a mammal in need threreof.  
     
     
       2. The method of claim  1 , wherein R 1  stands for ethyl. 
     
     
       3. The method of claim  1 , wherein R 1  stands for ethyl and Y stands for —O—. 
     
     
       4. The method of claim  1 , wherein R 2  stands for a lower alkoxycarbonyl group substituted with cyclohexyloxycarbonyloxy. 
     
     
       5. The method of claim  1 , wherein R 3  stands for one of the following:                    
     
     
       6. The method of claim  5 , wherein R 3  stands for tetrazolyl. 
     
     
       7. The method of claim  1 , wherein R 2  stands for a lower alkoxylcarbonyl group substituted with a cyclohexyloxycarbonyloxyl group and R 3  stands for a tetrazolyl group. 
     
     
       8. The method of claim  1 , wherein R 1  stands for a lower alkyl group; Y stands for —O—; R 2  stands for a lower alkoxycarbonyl group substituted with a cyclohexyloxycarbonyloxyl group; and R 3  stands for a tetrazolyl group. 
     
     
       9. The method of claim  1 , wherein said compound represented by formula (I′) is 2-ethoxy-1-[[2′-(1H-tetrazole-5yl)biphenyl-4-yl ]methyl]-1-benzimidazole-7-carboxyl acid. 
     
     
       10. The method of claim  1 , wherein said compound represented by formula (I′) is pivaloyloxymethyl 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate. 
     
     
       11. The method of claim  1 , wherein R 2  stands for a carboxyl group. 
     
     
       12. The method of claim  1 , wherein R 3  stands for 4,5-dihydro-5-oxo-1,2,4-oxadiazole-3-yl. 
     
     
       13. The method of claim  1 , wherein the method is a method of treatment. 
     
     
       14. The method of claim  1 , wherein said compound represented by formula (I′) is (±)-1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)-)biphenyl-4-yl]-1H-benzimidazole-7-carboxylate. 
     
     
       15. The method of claim  1 , wherein the diabetic nephropathy is diabetic nephropathy accompanying sclerosis of the glomeruli. 
     
     
       16. The method of claim  1 , wherein glomerulonephritis is glomerulonephritis accompany sclerosis of the glomeruli. 
     
     
       17. The method of claim  1 , wherein said compound represented by formula (I′) is 2-ethoxy-1-[[2′-(4,5dihydro-5-oxo-1,2,4-oxadiazole-3-yl)biphenyl-4-yl)]methyl]-1H-beanziradazole-7-carboxylic acid.

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